Abstract: Lithium salts with fluorinated chelated orthoborate anions are prepared and used as electrolytes or electrolyte additives in lithium-ion batteries. The lithium salts have two chelate rings formed by the coordination of two bidentate ligands to a single boron atom. In addition, each chelate ring has two oxygen atoms bonded to one boron atom, methylene groups bonded to the two oxygen atoms, and one or more fluorinated carbon atoms bonded to and forming a cyclic bridge between the methylene groups.

Abstract: Provided herein are methods of isolating a 4-chloro-2-fluoro-3-substituted-phenylboronic acid. The method comprises contacting a mixture of water, a water miscible organic solvent, and a 4-chloro-2-fluoro-3-substituted-phenylboronic acid with a salt to form a water miscible organic solvent layer and a water layer. The 4-chloro-2-fluoro-3-substituted-phenylboronic acid is partitioned into the water miscible organic solvent layer, which is separated from the water layer. Additional methods are disclosed, as is a 4-chloro-2-fluoro-3-substituted-phenylboronic acid produced by one of the methods, wherein the 4-chloro-2-fluoro-3-substituted-phenylboronic acid is obtained at a yield of greater than approximately 90%.

Abstract: Multi-functional additives which impart improved antioxidancy to lubricating oil compositions and frictional properties resulting in improved fuel economy in an internal combustion engine are disclosed. More particularly disclosed is a boron containing salt of an oil soluble hydroxylated amine and a hindered phenolic acid product prepared by: a) reacting an oil soluble hydroxylated amine of the general formula II: wherein A at each occurrence is each independently C2-C6 alkylene group; R is methyl or an alkyl or alkenyl group having C2-C24 carbon atoms; Y is hydrogen, C1-C6 alkyl group or A-OH; x is an integer of 1 or 2; and z is an integer of 0 or 1; with a boron containing compound under reactive conditions; and b) mixing the reaction product of step a) with a hindered phenolic acid.

Abstract: A protected organoboronic acid includes a boron having an sp3 hybridization, a conformationally rigid protecting group bonded to the boron, and an organic group bonded to the boron through a boron-carbon bond. A method of performing a chemical reaction includes contacting a protected organoboronic acid with a reagent, the protected organoboronic acid including a boron having an sp3 hybridization, a conformationally rigid protecting group bonded to the boron, and an organic group bonded to the boron through a boron-carbon bond. The organic group is chemically transformed, and the boron is not chemically transformed.

Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.

Abstract: Described herein are novel metal salts capable as nucleating agents for polyolefins. The present invention relates to such salts synthesized by reacting potassium hydroxide with carboxylic acids and further, to the achievement of high crystallization temperatures in polypropylene compositions upon dispersal therein of formulations containing one or more of the said metal salts.

Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.

Abstract: Disclosed are a phenylboronic acid monomer and a phenylboronic acid polymer, each of which can have a pKa value suitable for the use under physiological environments and can be used for various applications. The pheanylboronic acid monomer has a structure represented by formula (13) and therefore has high hydrophilicity, can have a satisfactorily low pKa value when the phenyl ring is fluorinated, and can have a polymerizable unsaturated bond. The phenylboronic acid monomer has high hydrophilicity at a pKa value of 7.4 or less which is a physiological level, and can be polymerized with a wide variety of monomers to produce polymers suitable for the intended purposes.

Abstract: Design of a disposable screen printed electrode (SPE) for sensing percentage glycated hemoglobin using electrochemistry is disclosed. SPE has four electrodes, one working electrode for the detection of glycated hemoglobin, one working electrode for the detection of hemoglobin and the other two electrodes are counter and reference electrodes that are common for both detection schemes. It also has a cellulose acetate membrane with lysis agents and surfactant embedded in it. Lysis agents lyse erythrocytes and release hemoglobin. Surfactants modify hemoglobin structure and enhance the rate the electron transfer and thereby the output signal during the electrochemical analysis. The SPE is low cost and user friendly. The only input from the user is a drop of blood.

Abstract: Provided are a sensing device and a biosensor that are capable of achieving stable performance in sensing saccharides or hydroxyl group-containing polymers, and that can be stored for a long time. The biosensor 8 of the present invention uses, as a component for sensing glucose, a sensing device 16 in which a completely synthetic phenylboronic acid compound 21 is bound without using enzymes that have been conventionally used. Consequently, the biosensor 8 can eliminate the problem of protein denaturation to achieve stable performance in sensing glucose, and it is possible to achieve the biosensor 8 can be stored for a long time.

Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. Another aspect of the invention provides for the use of the disclosed compounds for treating Type II diabetes, insulin resistance, glucose intolerance, hyperglycemia, hypoglycemia, hyperinsulinemia, obesity, hyperlipidemia, or hyperlipoproteinemia.

Abstract: Novel fluorescent dyes are disclosed for use in analyte detection. In particular, mono- and bis-substituted HPTS dyes and methods of making them are provided.

Abstract: The present invention relates to substituted benz[a]anthracene derivatives, to the preparation and use thereof in organic electroluminescent devices, and to organic electroluminescent devices, in particular blue-emitting devices, in which these compounds are used as matrix material or dopant in the emitting layer and/or as hole-transport material and/or as electron-transport material.

Abstract: Compounds according to Formula I are potent inhibitors of Arginase I and II activity: where R1, R2, R3, R4, D, W, X, Y, and Z are defined in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use in treating or preventing a disease or a condition associated with arginase activity.

Abstract: Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity: where R1, R2, R3, R4, R5, R6, R7, R8, R9, D, M, X, and Y are defined as set forth in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use for treating or preventing a disease or a condition associated with arginase activity.

Abstract: Compounds having enhanced oxidation stability are disclosed. The compounds have an aryl boronic acid residue having one or more electron withdrawing groups on the aromatic moiety which contains the boronic acid residue, such that the molecule has enhanced oxidation resistance as compared to a corresponding molecule without the one or more electron withdrawing groups.

Abstract: The present invention relates to nicotinamide derivatives of formula (I), to compositions containing same, and to the therapeutic use thereof, in particular as anticancer drugs. The invention also relates to the method for preparing said compounds, as well as to some of the intermediate products.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: The present invention relates to the process for preparing a boronic acid or ester chemically, in which an aromatic compound is reacted with a boronating agent, in the presence of magnesium metal (Mg0). The invention also relates to the boronic acids or esters that can be obtained by means of this process and to the use thereof for example as a synthesis intermediate, in the Suzuki reaction, in the pharmaceutical or alternatively electronics field.

Abstract: The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.

Abstract: A method for producing an organolithium compound includes the step of reacting an aromatic compound or a halogenated unsaturated aliphatic compound and a lithiating agent in the presence of a coordinating compound containing three or more elements having a coordinating ability in a molecule, at least one thereof being a nitrogen element, or a coordinating compound containing three or more oxygen elements having a coordinating ability in a molecule, at least one of the groups containing the oxygen elements having a coordinating ability being a tertiary alkoxy group, at a temperature of ?40° C. to 40° C.

Abstract: The present invention provides a protein cross-linking inhibitor containing a compound represented by any of the following formulas (1)-(13), or a pharmaceutically acceptable salt thereof: R3—[—X—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(1) R3—[—X—B(ZR1)—Y—]n—R4,??(2) R3—[—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(3) R3—[—X—B(ZR1)—]n—R4,??(4) R3—[—B(ZR2)—W—]n—R4,??(5) R3—X—B(ZR1)-T[B(ZR2)—W—R4]2,??(6) R3—B(OH)2,??(7) R3—B(ZR1)—X—B(ZR2)—R4,??(8) R3—B(R1)—O—B(R2)—R4,??(9) R3—[—X—B(ZR1)—Y—B(ZR2)—]n—R4,??(10) R3—[—X—B(ZR1)—Y—B(ZR2)—W-Q-]n—R4,??(11) R3—[—P—X—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(12) [R3—X—B(ZR1)—Y]2B(ZR2),??(13) wherein each symbol is as defined in the DESCRIPTION.

Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: Compounds having enhanced oxidation stability are disclosed. The compounds have an aryl boronic acid residue having one or more electron withdrawing groups on the aromatic moiety which contains the boronic acid residue, such that the molecule has enhanced oxidation resistance as compared to a corresponding molecule without the one or more electron withdrawing groups.

Abstract: The present invention provides a compound represented by the following general formula (I): or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing such a compound, and the like. The compound or a pharmaceutically acceptable salt thereof, the pharmaceutical composition containing such a compound, or the like is useful as a medicine or the like for therapy of benign prostatic hyperplasia, cancer, osteoporosis, psoriasis, secondary hyperparathyroidism, chronic glomerulonephritis, lupus nephritis and/or diabetic nephropathy and the like.

Abstract: A saccharide-measuring fluorescence sensor substance including a copolymer of at least the following two compounds (I) and (II) is provided: (I) a fluorescent monomer compound represented by the following formula (1): formula (1) wherein: Q, Q? and D3 may be the same or different, may be combined together into a fused ring, and are each a substituent selected from the group consisting of a hydrogen atom, a halogen atom, a hydroxyl group, and substituted or unsubstituted alkyl, acyl, oxyalkyl, carboxyl, carboxylate ester, carboxamido, cyano, nitro, amino and aminoalkyl groups; and D1, D2 and D4 each represent a substituent, wherein at least one of D1, D2 and D4 is a substituent group comprising a vinyl group at an end thereof, and wherein the substituent group comprising a vinyl group at an end thereof enables the fluorescent monomer compound to be soluble in water, and (II) at least one hydrophilic, polymerizable monomer having a vinyl group.

Abstract: Compounds having enhanced oxidation stability are disclosed. The compounds have an aryl boronic acid residue having one or more electron withdrawing groups on the aromatic moiety which contains the boronic acid residue, such that the molecule has enhanced oxidation resistance as compared to a corresponding molecule without the one or more electron withdrawing groups.

Abstract: This invention provides, among other things, novel compounds useful for treating bacterial infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.

Abstract: Disclosed herein are ?-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising ?-aminoboronic acids and methods of use thereof.

Abstract: Substituted aryl-boron compounds comprising at least one 18F atom, as illustrated by the formula (I), where at least one of Y1 or Y2 is 18F and A1 is a substituted aromatic ring, with G1-5 being, independently, C or N, and where the substitutents of the aromatic ring or polycyclic moiety (other than boron) comprise at least one electron-withdrawing group (EWG), providing that sigma total (?total) for all substituents on the aromatic ring or polycyclic moiety except B is about 0.06 or more when said at least one EWG is positioned ortho to B, or about 0.2 or more when no EWG is positioned ortho to B. The compounds include neutral (N=1) and ionic borate (N=2) embodiments. The compounds are useful as positron emission tomography (PET) imaging agents.

Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: The present disclosure describes operationally simple methods for the low temperature, catalytic activation of carboxylic acids for organic reactions, in particular for direct amidation reactions with amines. The methods involve the use of orthosubstituted arylboromc acids of the formula (I), wherein the groups R1 to R5 are as defined herein. In preferred embodiments R1 is halogen. The arylboromc acids catalyze nucleophilic 1,2-addition reactions, conjugate 1,4-addition reactions, and cycloaddition reactions, including Diels-Alder reactions involving ?,?-unsaturated carboxylic acids.

Abstract: The present invention is directed to arginase inhibitor compounds of formula IA or formula IB: or a pharmaceutically acceptable salt thereof, compositions containing these compounds, and methods of their use for the treatment and diagnosis of conditions characterized by upregulation of arginase, abnormally high arginase activity, or by abnormally low nitric oxide synthase activity.

Abstract: Disclosed herein are ?-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising ?-aminoboronic acids and methods of use thereof.

Abstract: Salts of a peptide boronic acid drug, for example of Cbz-(R)-Phe-(S)-Pro-(R)-Mpg-B(OH)2. The counter-ion to the boronate may be an alkali metal or derived from a strongly basic organic nitrogen-containing compound.

Abstract: One aspect of the present invention relates to inhibitors of post-pro line protease enzymes, such as inhibitors of dipeptidyl peptidase IV (DPIV). Other aspects of the invention relate to pharmaceutical compositions and methods of use thereof. In certain embodiments, a DPIV inhibitor comprises a carboxylic acid-containing side chain moiety at the P1 or P2 position or both. The inhibitors of the invention should possess improved specificity for the targeted protease and low toxicity.

Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: A new N-heterocyclic catalyst system which contains N-heterocyclic carbene and amido as ligands, which are strongly bound to a palladium metal. Another heteroatom functionality can be used as a third ligand L. The NHC-amidate ligand system is unique in structure, and shows excellent reactivities in a number of chemical reactions. The chemical reactions include carbon-carbon and carbon-heteroatom (oxygen and nitrogen) bond formations, and oxidation reactions of saturated carbon chemicals via C—H activation.

Abstract: Vitamin D derivatives, notably non-steroidal vitamin D derivatives, are prepared from novel disubstituted phenylboronic acid compounds having the formula (I): and also from the novel intermediates having the formulae (1), (2), (3) and (10):

Abstract: A process for the manufacture of aminocarbonyl boronic acids of formula (IV) by converting the compounds of formula (III) with a Brønsted base Y(OH)n in a solvent or a solvent mixture, in which Z represents an optionally substituted arylene, heteroarylene, alkene, heteroalkene, alkylidene, heteroalkylidene, alkenylidene, heteroalkenylidene, alkynylidene, arylalkylene, heteroarylalkylene, arylheteroalkylene, heteroarylheteroalkylene, alkylheteroarylene, heteroalkylheteroarylene, or alkylarylene group; Y represents a metal or ammonium cation of valence n with 0<n<5; and B represents boronic acid, boronic acid ester, or a borate, or a boronic acid anhydride. The aminocarbonyl boronic acids of formula (IV) can be further hydrolyzed to form the carboxy boronic acid of formula (V).

Abstract: The present invention is directed to novel compounds according to formula (I) wherein R1, R2, and X are as defined herein. The invention also discloses methods of preparation, pharmaceutical compositions, and methods of disease treatment utilizing pharmaceutical compositions comprising these compounds. The compounds of this invention are novel therapeutic agents for the treatment of cancer, diabetes, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. The invention also discloses pharmaceutical compositions and methods of treatment of disease in mammals.

Abstract: The present invention relates to novel boronic chalcone derivatives which are useful as antitumor/anticancer agents. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good inhibitors of the growth of human breast cancer cells. The present invention also relates to the use of the novel boronic chalcone derivatives to treat cancer. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of cancer.

Abstract: The present invention relates to the use of aromatic boronic acid or borinic acid derivatives in organic electronic devices, in particular electroluminescent devices.

Abstract: A fluorescent monomer compound represented by the following formula (1) is provided: wherein Q, Q? and D3 may be the same or different, may be combined together into a fused ring, and are each a substituent selected from the group consisting of a hydrogen atom, a halogen atom, a hydroxyl group, and substituted or unsubstituted alkyl, acyl, oxyalkyl, carboxyl, carboxylate ester, carboxamido, cyano, nitro, amino and aminoalkyl groups; and D1, D2 and D4 each represent a substituent, wherein at least one of D1, D2 and D4 is a substituent group comprising a vinyl group at an end thereof, and wherein the substituent group comprising a vinyl group at an end thereof enables the fluorescent monomer compound to be soluble in water.

Abstract: Thyronamine derivatives and analogs, methods of using such compounds, and pharmaceutical compositions containing them are disclosed.

Abstract: The present invention relates to novel boronic chalcone derivatives which are useful as antitumor/anticancer agents. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good inhibitors of the growth of human breast cancer cells. The present invention also relates to the use of the novel boronic chalcone derivatives to treat cancer. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of cancer.

Abstract: The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor that contain a carboxylic acid moiety. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.

Abstract: Systems and methods for detecting glucose in a sample using, for example, a regenerable sensor are described. The sensor may, for example, include boronic acid to detect with great sensitivity and at a low cost the glucose in the sample.

Abstract: A saccharide-measuring fluorescence sensor substance including a copolymer of at least the following two compounds (I) and (II) is provided: (I) a fluorescent monomer compound represented by the following formula (1): formula (1) wherein: Q, Q? and D3 may be the same or different, may be combined together into a fused ring, and are each a substituent selected from the group consisting of a hydrogen atom, a halogen atom, a hydroxyl group, and substituted or unsubstituted alkyl, acyl, oxyalkyl, carboxyl, carboxylate ester, carboxamido, cyano, nitro, amino and aminoalkyl groups; and D1, D2 and D4 each represent a substituent, wherein at least one of D1, D2 and D4 is a substituent group comprising a vinyl group at an end thereof, and wherein the substituent group comprising a vinyl group at an end thereof enables the fluorescent monomer compound to be soluble in water, and (II) at least one hydrophilic, polymerizable monomer having a vinyl group.

Abstract: The present invention relates to amorphous and polymorphic forms of sodium 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate and their use for facilitating the delivery of active agents, such as insulin, to a target.